Dosing & Uses
Dosage Forms & Strengths
capsule
- 25mg
- 50mg
Parkinson Disease
Indicated as an adjunct to levodopa/carbidopa to reduce OFF episodes in patients with Parkinson disease
50 mg PO qHS
Dosage Modifications
Renal impairment
- Mild-to-moderate (CrCl 30-89 mL/min): No dosage adjustment necessary
- Severe (CrCl<30 mL/min): Not studied; owing to the potential for increased exposure, monitor for adverse reactions and discontinue therapy if tolerability issues arise
- End-stage renal disease (ESRD) (CrCl <15 mL/min): Avoid use
Hepatic impairment
- Mild (Child-Pugh A): No dosage adjustment necessary
- Moderate (Child-Pugh B): 25 mg PO qHS
- Severe (Child-Pugh C): Avoid use
Dosing Considerations
When discontinuing therapy, monitor patients and consider adjustment of other dopaminergic therapies as needed
European Drug Information
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Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (3)
- isocarboxazid
opicapone, isocarboxazid. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and opicapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.
- phenelzine
opicapone, phenelzine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and opicapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.
- tranylcypromine
opicapone, tranylcypromine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Both nonselective MAO inhibitors and opicapone inhibit catecholamine metabolism, leading to increased levels of catecholamines. Potential for dangerously high HR or BP.
Serious - Use Alternative (0)
Monitor Closely (12)
- acrivastine
acrivastine and opicapone both increase sedation. Use Caution/Monitor.
- amisulpride
amisulpride and opicapone both increase sedation. Use Caution/Monitor.
- asenapine
asenapine and opicapone both increase sedation. Use Caution/Monitor.
- asenapine transdermal
asenapine transdermal and opicapone both increase sedation. Use Caution/Monitor.
- dobutamine
opicapone will increase the level or effect of dobutamine by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- dopamine
opicapone will increase the level or effect of dopamine by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- epinephrine
opicapone will increase the level or effect of epinephrine by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- epinephrine inhaled
opicapone will increase the level or effect of epinephrine inhaled by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- epinephrine racemic
opicapone will increase the level or effect of epinephrine racemic by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- isoproterenol
opicapone will increase the level or effect of isoproterenol by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- methyldopa
opicapone will increase the level or effect of methyldopa by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
- norepinephrine
opicapone will increase the level or effect of norepinephrine by decreasing metabolism. Use Caution/Monitor. Opicapone is a COMT inhibitor. Caution if coadministered with drugs metabolized by COMT. If coadministered, monitor for changes in heart rate, heart rhythm, and blood pressure.
Minor (0)
Adverse Effects
>10%
Dyskinesia (20%)
1-10%
Constipation (6%)
Increased blood creatine kinase (5%)
Hypotension/syncope (5%)
Decreased weight (4%)
Hypertension (3%)
Dry mouth (3%)
Dizziness (3%)
Hallucination (3%)
Warnings
Contraindications
Concomitant use of nonselective monoamine oxidase (MAO) inhibitors
History of pheochromocytoma, paraganglioma, or other catecholamine-secreting neoplasm
Cautions
Patients treated with dopaminergic medications and/or medications that increase levodopa exposure have reported falling asleep while engaged in activities of daily living (eg, operating motor vehicles); advise not to drive and to avoid other potentially dangerous activities
Hypotension (orthostatic and nonorthostatic), syncope, and presyncope occurred; monitor for hypotension; if hypotension occurs, consider discontinuing or adjusting dosage of other medications that may lower blood pressure
May potentiate the effects of levodopa and may cause or exacerbate dyskinesia; consider levodopa or dopaminergic medication dose reduction
Hallucinations, delusions, agitation, or aggressive behavior occurred; consider discontinuing if hallucinations or psychoticlike behaviors occur; avoid treating patients with a major psychotic disorder because of the risk of exacerbating the psychosis with an increase in central dopaminergic tone
May intensify urges (eg, gambling, increased sexual activity, spending, binge eating) and the inability to control these urges while taking one or more dopaminergic therapies that increase central dopaminergic tone; reevaluate and consider discontinuing therapy if urges develop during treatment
Symptoms resembling neuroleptic malignant syndrome (characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability), with no other obvious etiology, have been reported in association with rapid dose reduction, withdrawal of, or changes in drugs that increase central dopaminergic tone; when discontinuing therapy, monitor and consider adjustment of other dopaminergic therapies as needed
Drug interaction overview
- Opicapone is a substrate of P-gp, BCRP, MRP2, OATP1B2, and OATP2B1 transporters; no clinically significant transporter-mediated interaction is expected for opicapone
-
Nonselective MAO inhibitors
- Coadministration is contraindicated
- Concomitant use with nonselective MAO inhibitors (eg, phenelzine, isocarboxazid, tranylcypromine) may inhibit catecholamine metabolism, leading to increased levels of catecholamines
- Selective MAO-B inhibitors can be used concomitantly with opicapone
-
Drugs metabolized by catechol-O-methyltransferase (COMT)
- Use with caution
- Coadministration with drugs metabolized by COMT may affect the pharmacokinetics of those drugs, which may increase the risk of possible arrhythmias, increased heart rate, and excessive changes in blood pressure
- Monitor for changes in heart rate, rhythm, and blood pressure in patients concomitantly treated with opicapone and drugs metabolized by COMT
Pregnancy & Lactation
Pregnancy
No adequate data available on use in pregnant females
Animal data
- Oral administration during pregnancy resulted in adverse effects on embryofetal development (increased incidence of fetal abnormalities) at clinically relevant plasma exposure in one of two species tested
- In addition, opicapone is always coadministered with levodopa/carbidopa, which is known to cause development toxicity in rabbits
Lactation
No data available on drug presence in human milk and its effects on breastfeeding or milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Once daily, peripheral-acting, COMT inhibitor; decreases conversion rate of levodopa to 3-O-methyldopa, thereby prolonging levodopa half-life to reduce motor fluctuations
Absorption
Peak plasma time: 2 hr
Effects of food
- After a moderate-fat/moderate-calorie meal, mean peak plasma concentration decreased 62%, mean AUC decreased 31%, delayed peak plasma time by 4 hr
Distribution
Protein bound: >99% (independent of concentration)
Metabolism
Primary metabolic pathway: Sulphation
Other metabolic pathways: Glucuronidation, methylation (by COMT), reduction, and glutathione conjugation
Elimination
Mean half-life: 1-2 hr
Excretion
- Feces: 70% (22% unchanged)
- Expired: 20%
- Urine: 5% (<1 unchanged)
Administration
Oral Administration
Administer at bedtime
Do not eat food for 1 hr before and for at least 1 hr after administration
Missed dose: Take dose at the next scheduled time
Storage
Capsules: Store at <30ºC (86ºF)
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